RWJ-38063
Chemical Name: N-[2-[4-(2-Isopropoxyphenyl)piperazin-1-yl]ethyl]-2-(2-oxopiperidin-1-yl)acetamide
CAS No. 216252-56-1, 216252-58-3 (citrate (1:1))
项目整合开发状态: Preclinical
项目研究机构: Ortho-McNeil (Originator)
合成路线:The intermediate amine (IV) was prepared by alkylation of N-(2-isopropoxyphenyl)piperazine (I) with N-(2-bromoethyl)phthalimide (II),followed by removal of the phthaloyl group upon treatment with methylhydrazine.
合成路线:Alkylation of delta-valerolactam (V) with tert-butyl bromoacetate in the presence of NaH provided (VI).Subsequent tert-butyl ester cleavage by means of trifluoroacetic acid furnished 2-(2-oxopiperidin-1-yl)acetic acid (VII),which was finally coupled with amine (IV) to afford the title amide.
📌 参考资料/链接：
参考文献标题:Arylsubstd.piperazines useful in the treatment of benign prostatic hyperplasia
文献作者:Mulcahy,L.; Pulito,V.; Villani,F.; Li,X.; Murray,W.; Maryanoff,C.; Jolliffe,L.; Reitz,A.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:EP 0984777; US 6071915; WO 9851298
📄 详细内容
合成路线:The intermediate amine (IV) was prepared by alkylation of N-(2-isopropoxyphenyl)piperazine (I) with N-(2-bromoethyl)phthalimide (II),followed by removal of the phthaloyl group upon treatment with methylhydrazine.
合成路线:Alkylation of delta-valerolactam (V) with tert-butyl bromoacetate in the presence of NaH provided (VI).Subsequent tert-butyl ester cleavage by means of trifluoroacetic acid furnished 2-(2-oxopiperidin-1-yl)acetic acid (VII),which was finally coupled with amine (IV) to afford the title amide.
参考文献标题:Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists
文献作者:Li,X.; Murray,W.V.; Jolliffe,L.; Pulito,V.
参考来源:Bioorg Med Chem Lett 2000,10(10),1093
产品链接: CAS No. 216252-56-1››